Fatty Acid Amide Conjugates for Synergistic Anti-Inflammatory Delivery

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Solution Overview

Problem

Current treatments for various diseases such as autoimmune disorders, inflammatory diseases, and neurodegenerative conditions do not effectively target inflammation and oxidative stress, leading to inadequate therapeutic outcomes.

Innovation Solution

Development of fatty acid amides, specifically omega-3 fatty acid derivatives covalently linked with biologically active amines like cysteamine, glucosamine, dexpramipexole, and others, which are designed to be stable in plasma but release their components intracellularly in targeted tissues, enhancing delivery and biological activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If omega-3 fatty acids are administered alone or in non-covalent combination, then they provide basic anti-inflammatory effects, but they cannot achieve synergistic therapeutic effects and have limited tissue delivery efficiency

Engineering Contradiction:
Improvetherapeutic effectVSAvoidtissue delivery efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent combines omega-3 fatty acids with biologically active amines through covalent bonding to create fatty acid amide conjugates. This merging of two separate therapeutic agents into a single molecular entity enables synergistic anti-inflammatory and neuroprotective effects that cannot be achieved by administering the individual components separately, while also improving tissue delivery efficiency through the amine component's enhanced pharmacokinetic properties

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates composite molecular structures by covalently linking omega-3 fatty acid moieties with biologically active amine moieties. This composite approach integrates the anti-inflammatory properties of omega-3 fatty acids with the enhanced tissue penetration and stability of amine-containing compounds, producing a therapeutic agent with superior and synergistic biological activity

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If fatty acid amides are designed to be stable in plasma, then they maintain integrity during circulation, but they require specific intracellular conditions for hydrolysis and component release

Engineering Contradiction:
Improveplasma stabilityVSAvoidhydrolysis mechanism complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent designs fatty acid amides with plasma stability by selecting amine moieties and linkage structures that resist hydrolysis in the plasma environment. The conjugates remain stable during circulation until they reach intracellular environments where changes in pH, enzyme presence, or other parameters trigger hydrolysis and release of the active components, thus achieving both stability and controlled release

Inventive Principle:
Principle #35Parameter changes

3Reliability

If biologically active amines are coupled to omega-3 fatty acids, then synergistic biological effects are achieved, but the molecular structure and pharmacokinetic profile become more complex

Engineering Contradiction:
Improvebiological activityVSAvoidmolecular structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent employs biologically active amines that possess their own therapeutic properties in addition to serving as linkers for the fatty acid conjugates. These amine moieties contribute to the overall biological activity of the conjugate, providing multi-functional effects that enhance the therapeutic outcome while the modular design allows for systematic optimization of the molecular structure

Inventive Principle:
Principle #6Universality (Multi-functionality)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

These fatty acid amides demonstrate improved therapeutic effects by achieving synergistic anti-inflammatory and neuroprotective effects that cannot be replicated by administering individual components, effectively treating autoimmune, respiratory, and neurodegenerative diseases.

Implementation Method 1

in targeted tissues, intracellular enzymes will hydrolyze the fatty acid amides into the individual components, i.e. the omega-3 fatty acid and the amine moiety

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentEP2751071B1Fatty acid amides, compositions and methods of use
Publication Date: 2019.11.27 ASTRIA THERAPEUTICS INC
  • EP2751071B1 patent drawingFigure 1
  • EP2751071B1 patent drawingFigure 2
  • EP2751071B1 patent drawing

AI summary

The invention relates to fatty acid amides; compositions comprising an effective amount of a fatty acid amide; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a fatty acid amide.